4-[1-(4-Fluorobenzyl)-4-hydroxy-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acid as a prototype to develop dual inhibitors of HIV-1 integration process

2011 ◽  
Vol 92 (1) ◽  
pp. 102-107 ◽  
Author(s):  
Laura De Luca ◽  
Rosaria Gitto ◽  
Frauke Christ ◽  
Stefania Ferro ◽  
Sara De Grazia ◽  
...  
Keyword(s):  
Enoic Acid ◽  
Integration Process ◽  
Dual Inhibitors ◽  
Hiv 1

Diketoacid chelating ligands as dual inhibitors of HIV-1 integration process

2014 ◽  
Vol 78 ◽  
pp. 425-430 ◽  
Author(s):  
Dominga Rogolino ◽  
Mauro Carcelli ◽  
Carlotta Compari ◽  
Laura De Luca ◽  
Stefania Ferro ◽  
...  
Keyword(s):  
Chelating Ligands ◽  
Integration Process ◽  
Dual Inhibitors ◽  
Hiv 1

Design, synthesis and biological evaluation of caffeoyl benzanilides as dual inhibitors of HIV integrase and CCR5

MedChemComm ◽  
2016 ◽  
Vol 7 (10) ◽  
pp. 2028-2032 ◽  
Author(s):  
Xuefeng Sun ◽  
Ningning Fan ◽  
Weisi Xu ◽  
Yixing Sun ◽  
Xin Xie ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Hiv Integrase ◽  
Dual Inhibitor ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

Novel series of caffeoyl benzanilides have been synthesized and evaluated as dual inhibitors of HIV-1 CCR5/IN. Compound 9a exhibited the possibility of being a dual inhibitor of HIV-1.

Discovery of dual inhibitors targeting both HIV-1 capsid and human cyclophilin A to inhibit the assembly and uncoating of the viral capsid

2009 ◽  
Vol 17 (8) ◽  
pp. 3177-3188 ◽  
Author(s):  
Jiebo Li ◽  
Zhiwu Tan ◽  
Shixing Tang ◽  
Indira Hewlett ◽  
Ruifang Pang ◽  
...  
Keyword(s):  
Cyclophilin A ◽  
Viral Capsid ◽  
Dual Inhibitors ◽  
Hiv 1

Advances in rationally designed dual inhibitors of HIV-1 reverse transcriptase and integrase

2016 ◽  
Vol 24 (21) ◽  
pp. 5007-5016 ◽  
Author(s):  
Shuang-Xi Gu ◽  
Ping Xue ◽  
Xiu-Lian Ju ◽  
Yuan-Yuan Zhu
Keyword(s):  
Reverse Transcriptase ◽  
Dual Inhibitors ◽  
Hiv 1

scholarly journals Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain

2015 ◽  
Vol 58 (4) ◽  
pp. 1915-1928 ◽  
Author(s):  
Giuliana Cuzzucoli Crucitti ◽  
Mathieu Métifiot ◽  
Luca Pescatori ◽  
Antonella Messore ◽  
Valentina Noemi Madia ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Structure Activity Relationship ◽  
Ribonuclease H ◽  
Activity Relationship ◽  
Structure Activity ◽  
Dual Inhibitors ◽  
Relationship Of ◽  
Hiv 1

Fullerene derivatives as dual inhibitors of HIV-1 reverse transcriptase and protease

2021 ◽  
Vol 31 ◽  
pp. 127675
Author(s):  
Takumi Yasuno ◽  
Tomoyuki Ohe ◽  
Hiroki Kataoka ◽  
Kosho Hashimoto ◽  
Yumiko Ishikawa ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Fullerene Derivatives ◽  
Dual Inhibitors ◽  
Hiv 1

Antiretroviral effect simulation from black tea (Camellia sinensis) via dual inhibitors mechanism in HIV-1 and its social perspective in Indonesia

2021 ◽  
Vol 14 (1) ◽  
pp. 455-460
Author(s):  
Viol Dhea Kharisma ◽  
Sasando Dhohan Kharisma ◽  
Arif Nur Muhammad Ansori ◽  
Hanny Priskila Kurniawan ◽  
Adiana Mutamsari Witaningrum ◽  
...  
Keyword(s):  
Camellia Sinensis ◽  
Black Tea ◽  
Social Perspective ◽  
Dual Inhibitors ◽  
Hiv 1

Design, Synthesis, and Biological Evaluation of 1,3-Diarylpropenones as Dual Inhibitors of HIV-1 Reverse Transcriptase

ChemMedChem ◽  
2014 ◽  
pp. n/a-n/a ◽  
Author(s):  
Rita Meleddu ◽  
Valeria Cannas ◽  
Simona Distinto ◽  
Giorgia Sarais ◽  
Claudia Del Vecchio ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Hiv 1

scholarly journals Evidence that Stable Retroviral Transduction and Cell Survival following DNA Integration Depend on Components of the Nonhomologous End Joining Repair Pathway

2004 ◽  
Vol 78 (16) ◽  
pp. 8573-8581 ◽  
Author(s):  
René Daniel ◽  
James G. Greger ◽  
Richard A. Katz ◽  
Konstantin D. Taganov ◽  
Xiaoyun Wu ◽  
...  
Keyword(s):  
Dna Repair ◽  
Nonhomologous End Joining ◽  
Transduction Efficiency ◽  
Repair Pathway ◽  
Integration Process ◽  
End Joining ◽  
General Role ◽  
Dna Integration ◽  
Ligase Iv ◽  
Hiv 1

ABSTRACT We have previously reported several lines of evidence that support a role for cellular DNA repair systems in completion of the retroviral DNA integration process. Failure to repair an intermediate in the process of integrating viral DNA into host DNA appears to trigger growth arrest or death of a large percentage of infected cells. Cellular proteins involved in the nonhomologous end joining (NHEJ) pathway (DNA-PKCS) and the damage-signaling kinases (ATM and ATR) have been implicated in this process. However, some studies have suggested that NHEJ proteins may not be required for the completion of lentiviral DNA integration. Here we provide additional evidence that NHEJ proteins are required for stable transduction by human immunodeficiency type 1 (HIV-1)-based vectors. Our analyses with two different reporters show that the number of stably transduced DNA-PKCS-deficient scid fibroblasts was reduced by 80 to 90% compared to the number of control cells. Furthermore, transduction efficiency can be restored to wild-type levels in scid cells that are complemented with a functional DNA-PKCS gene. The efficiency of stable transduction by an HIV-1-based vector is also reduced upon infection of Xrcc4 and ligase IV-deficient cells, implying a role for these components of the NHEJ repair pathway. Finally, we show that cells deficient in ligase IV are killed by infection with an integrase-competent but not an integrase-deficient HIV-1 vector. Results presented in this study lend further support to a general role for the NHEJ DNA repair pathway in completion of the retroviral DNA integration process.

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